Xanomeline (oxalate) [141064-23-5]

Referência HY-13410-1ml

Tamanho : 10mM/1mL

Marca : MedChemExpress

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Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease.

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Xanomeline oxalate Chemical Structure

Xanomeline oxalate Chemical Structure

CAS No. : 141064-23-5

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Based on 1 publication(s) in Google Scholar

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Description

Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease[1].

IC50 & Target

muscarinic receptor[1]

In Vitro

Xanomeline stimulates phosphoinositide (PI) hydrolysis in the A9 L m1 cells[1].
Xanomeline inhibits [3H]-pirenzepine ([3H]-PZ) and [3H]-oxotremorine-M ([3H]-OXO-M) binding to rat brain with Kis of 7 and 3 nM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Xanomeline robustly stimulates in vivo PI hydrolysis and the effect is blocked by muscarinic antagonists, demonstrating mediation by muscarinic receptors. In mice the ED100 for Xanomeline-induced stimulation of [3H]-IP accumulation is 54 μmole/kg in hippocampus. And in rats the ED100 for Xanomeline-induced stimulation of [3H]-IP accumulation is 8.1 μmole/kg in hippocampus[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CF1 mice weighing 18-20 g are injected [3H]-myoinositol[1]
Dosage: 8.1-81 μmole/kg
Administration: S.c. injections; 1 h prior to killing and 1 h after the administration
Result: Increased accumulation in a dose-related manner up to 130%, 75%, 60% above lithium levels in hippocampus, cortex and neostriatum, respectively. And did not increase accumulation of [3H]-IP in the brain stem. Induced salivation, tremor and hypothermia in mice with the ED50 of 13.7±0.8 μmole/kg.
Animal Model: Rats are injected [3H]-myoinositol[1]
Dosage: 2.7-81 μmole/kg
Administration: S.c. injections; 1 h prior to killing and 1 h after the administration
Result: Increased [3H]-IP formation dose dependently in hippocampus up to 221% above lithium control.
Essai clinique
Masse moléculaire

371.45

Formule

C16H25N3O5S

CAS No.

141064-23-5

Appearance

Solid

Color

White to off-white

SMILES

CN1CCC=C(C2=NSN=C2OCCCCCC)C1.O=C(O)C(O)=O

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvant et solubilité
In Vitro: 

DMSO : 50 mg/mL (134.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6922 mL 13.4608 mL 26.9215 mL
5 mM 0.5384 mL 2.6922 mL 5.3843 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation

Purity: 99.89%

Références
  • [1]. F P Bymaster, et al. Xanomeline Compared to Other Muscarinic Agents on Stimulation of Phosphoinositide Hydrolysis in Vivo and Other Cholinomimetic Effects. Brain Res. 1998 Jun 8; 795(1-2):179-90.  [Content Brief]

  • [1]. F P Bymaster, et al. Xanomeline Compared to Other Muscarinic Agents on Stimulation of Phosphoinositide Hydrolysis in Vivo and Other Cholinomimetic Effects. Brain Res. 1998 Jun 8; 795(1-2):179-90.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6922 mL 13.4608 mL 26.9215 mL 67.3038 mL
5 mM 0.5384 mL 2.6922 mL 5.3843 mL 13.4608 mL
10 mM 0.2692 mL 1.3461 mL 2.6922 mL 6.7304 mL
15 mM 0.1795 mL 0.8974 mL 1.7948 mL 4.4869 mL
20 mM 0.1346 mL 0.6730 mL 1.3461 mL 3.3652 mL
25 mM 0.1077 mL 0.5384 mL 1.0769 mL 2.6922 mL
30 mM 0.0897 mL 0.4487 mL 0.8974 mL 2.2435 mL
40 mM 0.0673 mL 0.3365 mL 0.6730 mL 1.6826 mL
50 mM 0.0538 mL 0.2692 mL 0.5384 mL 1.3461 mL
60 mM 0.0449 mL 0.2243 mL 0.4487 mL 1.1217 mL
80 mM 0.0337 mL 0.1683 mL 0.3365 mL 0.8413 mL
100 mM 0.0269 mL 0.1346 mL 0.2692 mL 0.6730 mL
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Xanomeline oxalate Related Classifications

Help & FAQs

Keywords:

Xanomeline141064-23-5LY246708LY 246708LY-246708mAChRMuscarinic acetylcholine receptorSMRAphosphoinositideAlzheimerdiseaseInhibitorinhibitorinhibit

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